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    • 7. 发明授权
    • 6-Aza-3H-1,4-benzodiazepines
    • 6-氮杂-3H-1,4-苯并二氮杂
    • US4008223A
    • 1977-02-15
    • US507605
    • 1974-09-19
    • Walter Von BebenburgHeribert Offermanns
    • Walter Von BebenburgHeribert Offermanns
    • C07D471/04
    • There are produced 6-aza-3H-1, 4-benzodiazepines and 6-aza-1,2-dihydro-3H-1,4-benzodiazepines of the formula ##STR1## where R.sub.1 is a halogen, R.sub.2 and R.sub.3 are hydrogen, halogen, trifluoromethyl, nitro, nitrile, hydroxy, lower alkyl, lower alkoxy, R.sub.4 is hydrogen, hydroxyl, hydroxyl acylated with a mono or dicarboxylic aid of 2 to 6 carbon atoms, lower alkoxy, lower alkyl, benzyl, lower aliphatic acyl, carboxy or carb-lower alkoxy, Z is nitrogen or NO, R.sub.5 is hydrogen, lower alkyl, lower alkyl substituted with cycloalkyl of 3 to 6 carbon atoms, lower alkenyl, cycloalkyl of 3 to 6 carbon atoms , lower hydroxyalkyl, benzyl, aliphatic acyl of 2 to 6 carbon atoms aminoalkyl of 2 to 7 carbon atoms, mono or di lower alkyl substituted aminoalkyl of 2 to 7 carbon atoms, lower alkyl substituted with 5 to 7 membered N-heterocyclic ring, containing 0 to 1 additional nitrogen or oxygen atoms, and A is oxygen, sulfur, =NR.sub.5, =NOR.sub.5, =NH-NHR.sub.5 or two hydrogen atoms and the --N(R.sub.5)--C--(=A)-- can also be in the tautomeric form --N=C(AR.sub.5) 13 and pharmacologically acceptable salts thereof. The compounds have spasmolytic, antiphlogistic and tranquilizer activity.
    • 产生式“IMAGE”的6-氮杂-3H-1,4-苯并二氮杂和6-氮杂-1,2-二氢-3H-1,4-苯并二氮杂其中R 1是卤素,R 2和R 3是氢, 卤素,三氟甲基,硝基,腈,羟基,低级烷基,低级烷氧基,R 4是氢,羟基,用2至6个碳原子的单或二羧酸酰化的羟基,低级烷氧基,低级烷基,苄基,低级脂族酰基,羧基 或碳 - 低级烷氧基,Z为氮或NO,R5为氢,低级烷基,被3至6个碳原子的环烷基取代的低级烷基,低级烯基,3至6个碳原子的环烷基,低级羟基烷基,苄基,脂族酰基 2至6个碳原子,2至7个碳原子的氨基烷基,2至7个碳原子的一或二低级烷基取代的氨基烷基,由5至7元N-杂环取代的低级烷基,含有0至1个额外的氮或氧原子, 并且A是氧,硫,= NR5,= NOR5,= NH-NHR5或两个氢原子,-N(R5)-C-(= A) - 也可以是τ 多晶型-N = C(AR5)13及其药理学上可接受的盐。 这些化合物具有解痉,消炎和镇静作用。
    • 9. 发明授权
    • N-Substituted .alpha.-ketocarboxylic acid amides
    • N-取代的α-酮羧酸酰胺
    • US4228082A
    • 1980-10-14
    • US56084
    • 1979-07-09
    • Axel KleemannHerbert KlenkHeribert OffermannsPaul ScherberichWerner Schwarze
    • Axel KleemannHerbert KlenkHeribert OffermannsPaul ScherberichWerner Schwarze
    • A01N25/00A01P3/00A01P13/00C07C67/00C07C231/00C07C231/06C07C231/08C07C235/72C07D307/54C07C103/737C07C103/76
    • C07D307/54
    • Compounds are prepared of the formula ##STR1## where R' is a t-alkyl group having 4 to 18 carbon atoms, preferably t-butyl, t-amyl or t-octyl and R is a straight or branched chain alkyl group with 1 to 18 carbon atoms, preferably 1 to 10 carbon atoms or an alkyl group substituted with one or more phenyl group or a halogen atom, particularly a chlorine atom, or a cycloalkyl group with 3 to 8 carbon atoms, particularly cyclopropyl, which can be substituted by one or more 1 to 3 carbon atom alkyl groups or one or more halogen atoms, preferably chlorine, or phenyl or naphthyl or a five membered heterocyclic group or such phenyl, naphthyl or heterocyclic group substituted by halogen atoms, nitro groups, alkyl or alkoxy with 1 to 5 carbon atoms by condensing in acid medium an acyl cyanide of the formulaR--CO--CN (II)where R is as defined above with either(a) a tertiary alcohol of the formulaHO--R' (III) in which R' is as defined above, or preferably(b) an alkene of the formula ##STR2## where R.sub.1 and R.sub.2 are the same or different and are hydrogen or an alkyl group and wherein R.sub.3 and R.sub.4 are the same or different and wherein the alkyl groups in each case can be 1 to 15 carbon atoms. Some of the compounds are new. They are useful as intermediates for synthesizing herbicides and can be used directly as fungicides.
    • 化合物由式(I)制备,其中R'是具有4至18个碳原子的叔烷基,优选叔丁基,叔戊基或叔辛基,R是直链或支链烷基 具有1至18个碳原子,优选1至10个碳原子的烷基或被一个或多个苯基或卤素原子,特别是氯原子或具有3至8个碳原子的环烷基特别是环丙基取代的烷基,其可以 被一个或多个1至3个碳原子的烷基或一个或多个卤素原子,优选氯,或苯基或萘基或五元杂环基或被卤素原子取代的苯基,萘基或杂环基,硝基,烷基 或具有1至5个碳原子的烷氧基,通过在酸性介质中缩合式R-CO-CN(II)的酰基氰,其中R如上定义,与(a)式HO-R'(III ),其中R'如上所定义,或优选(b)下式的烯烃(I) V)其中R 1和R 2相同或不同并且是氢或烷基,并且其中R 3和R 4相同或不同,并且其中每种情况下的烷基可以是1至15个碳原子。 一些化合物是新的。 它们可用作合成除草剂的中间体,可直接用作杀真菌剂。